7 results about "Thioredoxin reductase" patented technology

The present application relates to the chemical medicine field, specifically, it relates to a kind of anti-tumor calophyllol derivative, preparation method and application, the calophyllol derivative has good inhibitory effect on thioredoxin reductase activity, and it is found that the molecule inhibits the activity of thioredoxin reductase by inhibiting the selenium cysteine of thioredoxin reductase carbon end, and then kills tumor cell, and then obtain the anti-tumor candidate drug with higher activity and better pharmacokinetic characteristics.

This disclosure provides an E. coli strain, which lacks thioredoxin reductase activity encoded by trxB and thioredoxin 1 activity encoded by trxA, and glutathione reductase activity encoded by gor. Said E. coli strain expresses a mutated AhpC protein having glutathione reductase activity and a cytosolic prokaryotic disulfide isomerase. The E. coli strain has an oxidative cytosol and can be used to efficiently produce proteins having disulfide bonds.

An enzyme for reducing cystine to cysteine is a fusion protein that includes the protein activities of thioredoxin (protein i) having KEGG database number EC 1.8.4.8 or EC 1.8.4.10 and thioredoxin reductase (protein ii) having KEGG database number EC 1.8.1.9. The thioredoxin (protein i) is the protein activity of thioredoxin 1 from E. coli and the thioredoxin reductase (protein ii) is the protein activity of the thioredoxin reductase from E. coli. The activity of the fusion protein is at least 100% of the activity of a mixture of the same but unfused individual proteins i and ii. The fusion protein has the enzyme activity to reduce cystine to cysteine. The coding sequences (cds) responsible for the activity of protein i and ii has been fused.

The invention discloses thioredoxin reductase BrgTrxR, the amino acid sequence of the thioredoxin reductase BrgTrxR is shown as SEQ ID NO: 1, the gene is obtained from a Brevibacillus gelatini LD5 strain, the protease is subjected to heterologous expression through a genetic engineering means, the protease is purified through a nickel column and is mixed with keratinase BrgM4 to degrade chicken feather, experimental data shows that the activity of the reductase reaches 15.81 U / mg after the reductase is separated and purified, and the activity of the reductase reaches 15.81 U / mg after the reductase is mixed with keratinase BrgM4. In a mixed degradation system with the temperature of 40-80 DEG C and the pH value of 6.5-7.5, the thioredoxin reductase BrgTrxR can improve the hydrolytic activity of the keratinase BrgM4, after the chicken feather is degraded for 48 h through the synergistic effect of the two enzymes, the concentration of soluble protein reaches 14.45 mg / mL, and the thioredoxin reductase is beneficial to cooperating with the keratinase to improve the keratin degradation efficiency.

The invention relates to the technical field of preparation of anti-cancer drugs, in particular to a Schiff base gold (III) compound and a preparation method and application thereof.The series of symmetric or asymmetric Schiff base gold (III) compounds are synthesized on the basis of the bioisostere principle in combination with a Schiff base ligand, the cyclohexanediamine structure and the NNOO coordination mode of oxaliplatin are reserved, platinum (II) is replaced with gold (III), and the Schiff base gold (III) compound is synthesized. Meanwhile, the invention relates to application of the Schiff base gold (III) compound in preparation of anti-hepatoma drugs, the defects that oxaliplatin is strong in side effect and the like are overcome, in-vivo and in-vitro experiment results of the Schiff base gold (III) compound provided by the invention show that the compounds Au3 and Au7 are remarkable in anti-hepatoma activity and can target thioredoxin reductase (TrxR) and mitochondrial DNA (mtDNA) at the same time, and the Schiff base gold (III) compound can be used for preparing anti-hepatoma drugs. The further mechanism research shows that the compound can promote the generation of reactive oxygen species (ROS) to cause endoplasmic reticulum stress (ERS) and mitochondrial injury and finally induce pyroptosis and immunogenic cell death, and has great application potential.

This invention belongs to the field of medicinal chemistry and pharmaceutical technology, and discloses a pyrano[2,3-a]phenazine derivative, its preparation method, and its application in the preparation of anti-glioma drugs. The structural formula of the pyrano[2,3-a]phenazine derivative is as follows: R1 is H, halogen, or -N(C2H5)2; R2 is H or halogen; R3 is H, halogen, or -CH3; R4 is H or halogen; R5 is H, halogen, or -OCH3; R6 is H, halogen, -CH3, -C2H5, or -OCH3; R7 is H or -OCH3; X is -CN or -COOC2H5. This invention also discloses the preparation method of this pyrano[2,3-a]phenazine derivative and its application in the preparation of anti-glioma drugs. This type of compound has a strong inhibitory effect on thioredoxin reductase (TrxR) and significant inhibitory activity against human glioma cells (U87), showing great application potential in the preparation of anti-glioma drugs.

The invention discloses a preparation method and application of prodrugs CPT-40 and CPT-38 based on camptothecin, and belongs to the technical field of medicines. The invention aims to solve the technical problems of poor water solubility, low in-vivo stability and large toxic and side effects of the existing camptothecin drugs. The key point of the technical scheme of the invention is to provide a CPT-40 compound as shown in a formula (I) and a CPT-38 compound as shown in a formula (II), a preparation method of the CPT-40 compound and the CPT-38 compound, and application of the CPT-40 compound and the CPT-38 compound in preparation of antitumor drugs. The prodrug can be specifically activated by thioredoxin reductase highly expressed in tumor tissues to release active camptothecin so as to kill tumor cells. The compound is mainly used for preparing drugs for targeted therapy of tumors, and has the advantages of high selectivity, good plasma stability and high oral bioavailability.